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Medchemexpress/Metformin hydrochloride(Synonyms: 1,1-Dimethylbiguanide hydrochloride)/HY-17471A/10g188bio精品生物—专注于实验室精品爆款的电商平台 - 蚂蚁淘旗下精选188款生物医学科研用品
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Medchemexpress/Metformin hydrochloride(Synonyms: 1,1-Dimethylbiguanide hydrochloride)/HY-17471A/10g

Metformin(hydrochloride)isafirst-linedrugforthetreatmentoftype2diabetesandthereisincreasingevidenceofapotentialefficacyofthisagentasananti-cancerdrug.

CustomerValidation

  • MolCellProteomics.2017Jul;16(7):1324-1334.
  • MolNeurobiol.2016May11.
  • MolOncol.2017Aug;11(8):1035-1049.
  • CellPhysiolBiochem.2017Nov30;44(4):1381-1395.
  • BiochemPharmacol.2017Aug15;138:49-60.
  • JCellMolMed.2017Jul12.
  • FrontPharmacol.2016Oct20;7:390.
Description

Metformin(hydrochloride)isafirst-linedrugforthetreatmentoftype2diabetesandthereisincreasingevidenceofapotentialefficacyofthisagentasananti-cancerdrug.

InVitro

MetformininhibitsproliferationofESCsinaconcentration-dependentmanner.TheIC50is2.45 mMforA-ESCsand7.87 mMforN-ESCs.MetforminshowspronouncedeffectsonactivationofAMPKsignalinginA-ESCsfromsecretoryphasethanincellsfromproliferativephase[3].Metformin(0-500μM)decreasesglycogensynthesisinadose-dependentmannerwithanIC50valueof196.5μMinculturedrathepatocytes[4].MetforminshowscellviABIlityandcytotoxiceffectsonPC-3cellswithIC50of5mM[5].

InVivo

Metformin(100mg/kg,p.o.)alone,andmetformin(25,50,100mg/kg)withisoproterenolgroupsattenuatesmyocytenecrosisthroughhistopathologicalanalysis[1].Metformin(>900mg/kg/day,p.o.)resultsinmoribundity/mortalityandclinicalsignsoftoxicityinCrl:CD(SD)rats[2].

ClinicalTrial
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References
  • [1].SorayaH,etal.Acutetreatmentwithmetforminimprovescardiacfunctionfollowingisoproterenolinducedmyocardialinfarctioninrats.PharmacolRep.2012;64(6):1476-84.

    [2].QuaileMP,etal.Toxicityandtoxicokineticsofmetformininrats.ToxicolApplPharmacol.2010Mar15;243(3):340-7.

    [3].XueJ,etal.MetformininhibitsgrowthofeutopicstromalcellsfromadenomyoticendometriumviaAMPKactivationandsubsequentinhibitionofAKTphosphorylation:apossIBLeroleinthetreatmentofadenomyosis.Reproduction.2013Aug21;146(4):397-406.

    [4].OttoM,etal.Metformininhibitsglycogensynthesisandgluconeogenesisinculturedrathepatocytes.DiabetesObesMetab.2003May;5(3):189-94.

    [5].AvciCB,etal.Therapeuticpotentialofananti-diabeticdrug,metformin:alterationofmiRNAexpressioninprostatecancercells.AsianPacJCancerPrev.2013;14(2):765-8.

    [6].NieL,etal.TheLandscapeofHistoneModificationsinaHigh-FatDiet-InducedObese(DIO)MouseModel.MolCellProteomics.2017Jul;16(7):1324-1334.

    [7].ZhangD,etal.MetforminamelioratesBSCBdisruptionbyinhibitingneutrophilinfiltrationandMMP-9expressionbutnotdirectTJproteinsexpressionregulation.JCellMolMed.2017Jul12.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM6.0379mL30.1896mL60.3792mL
5mM1.2076mL6.0379mL12.0758mL
10mM0.6038mL3.0190mL6.0379mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

Metforminisdissolvedindouble-distilledwateratastockconcentrationof10mMandstoredat4°C. 

ESCsareplatedin96-wellplatesataconcentrationof1×103cells/well.Afterattachment,cellsaretreatedwithdifferentdosesofmetformin/compoundCfor0min,15min,1h,and24h.MTTassaysareperformedasdescribedpreviously.Inbrief,MTT(5mg/mL)isaddedtothe96-wellplatesatavolumeof10μL/well,andtheplatesareincubatedfor4h.TheMTTreactionisterminatedbyremovaloftheculturemediumcontainingMTT,and100μLDMSOperwellareaddedandincubatedatRTonashakerfor10mintoensurethatthecrystalshaddissolvedsufficiently.Absorbancevaluesaremeasuredat595nm.Cellproliferation(percentageofcontrol)iscalculatedasfollows:absorbance(experimentalgroup)/absorbance(controlgroup).Cellproliferationinhibition(percentageofcontrol)iscalculatedasfollows:100%−cellproliferation(percentageofcontrol).Eachexperimentisperformedinduplicateandrepeatedsixtimestoassessresultconsistency.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

Metformin(hydrochloride)isdissolvedinphysiologicalsaline.

Theanimalsarerandomizedintosixgroupsconsistingofsixratseach.Ratsingroup1(control)receivesasubcutaneousinjectionofphysiologicalsaline(0.5mL)andareleftuntreatedfortheentireexperimentalperiod.Ratsingroup2receivesanoraladministrationofmetformin(100mg/kg;twicedaily)for2daysandaresubcutaneouslyinjectedwithsalineatanintervalof24hfor2consecutivedays.Ratsingroup3(MIcontrol)receivesanoraladministrationofsaline(twicedaily)for2daysandarescinjectedwithisoproterenol(100mg/kg)dailyfor2consecutivedaysatanintervalof24h.Ratsingroups4to6aretreatedwithmetforminat25,50,and100mg/kg.Metforminisdissolvedinsalineandisgavagedatavolumeof0.25-0.5mLtwiceadayatanintervalof12h,startedimmediatelybeforeisoproterenolinjection.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].SorayaH,etal.Acutetreatmentwithmetforminimprovescardiacfunctionfollowingisoproterenolinducedmyocardialinfarctioninrats.PharmacolRep.2012;64(6):1476-84.

    [2].QuaileMP,etal.Toxicityandtoxicokineticsofmetformininrats.ToxicolApplPharmacol.2010Mar15;243(3):340-7.

    [3].XueJ,etal.MetformininhibitsgrowthofeutopicstromalcellsfromadenomyoticendometriumviaAMPKactivationandsubsequentinhibitionofAKTphosphorylation:apossibleroleinthetreatmentofadenomyosis.Reproduction.2013Aug21;146(4):397-406.

    [4].OttoM,etal.Metformininhibitsglycogensynthesisandgluconeogenesisinculturedrathepatocytes.DiabetesObesMetab.2003May;5(3):189-94.

    [5].AvciCB,etal.Therapeuticpotentialofananti-diabeticdrug,metformin:alterationofmiRNAexpressioninprostatecancercells.AsianPacJCancerPrev.2013;14(2):765-8.

    [6].NieL,etal.TheLandscapeofHistoneModificationsinaHigh-FatDiet-InducedObese(DIO)MouseModel.MolCellProteomics.2017Jul;16(7):1324-1334.

    [7].ZhangD,etal.MetforminamelioratesBSCBdisruptionbyinhibitingneutrophilinfiltrationandMMP-9expressionbutnotdirectTJproteinsexpressionregulation.JCellMolMed.2017Jul12.

MolecularWeight

165.62

Formula

C₄H₁₂ClN₅

CASNo.

1115-70-4

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

H2O:≥32mg/mL;DMSO:≥1.7mg/mL

Metforminhydrochlorideispreparedin0.5%methylcellulose[6].
Metforminhydrochlorideisdilutedwithnormalsaline,toachieveafinalmetforminconcentrationof20mg/mL[7].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References
  • [1].SorayaH,etal.Acutetreatmentwithmetforminimprovescardiacfunctionfollowingisoproterenolinducedmyocardialinfarctioninrats.PharmacolRep.2012;64(6):1476-84.

    [2].QuaileMP,etal.Toxicityandtoxicokineticsofmetformininrats.ToxicolApplPharmacol.2010Mar15;243(3):340-7.

    [3].XueJ,etal.MetformininhibitsgrowthofeutopicstromalcellsfromadenomyoticendometriumviaAMPKactivationandsubsequentinhibitionofAKTphosphorylation:apossibleroleinthetreatmentofadenomyosis.Reproduction.2013Aug21;146(4):397-406.

    [4].OttoM,etal.Metformininhibitsglycogensynthesisandgluconeogenesisinculturedrathepatocytes.DiabetesObesMetab.2003May;5(3):189-94.

    [5].AvciCB,etal.Therapeuticpotentialofananti-diabeticdrug,metformin:alterationofmiRNAexpressioninprostatecancercells.AsianPacJCancerPrev.2013;14(2):765-8.

    [6].NieL,etal.TheLandscapeofHistoneModificationsinaHigh-FatDiet-InducedObese(DIO)MouseModel.MolCellProteomics.2017Jul;16(7):1324-1334.

    [7].ZhangD,etal.MetforminamelioratesBSCBdisruptionbyinhibitingneutrophilinfiltrationandMMP-9expressionbutnotdirectTJproteinsexpressionregulation.JCellMolMed.2017Jul12.

Purity:99.08%

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